Bacterial translation inhibitors, 1-acylindazol-3-ols as anthranilic acid mimics.
The discovery and initial optimization of a novel anthranilic acid derived class of antibacterial agents has been described in a recent series of papers. This paper describes the discovery of 1-acylindazol-3-ols as a novel bioisostere of an anthranilic acid. The synthesis and structure-activity relationships of the indazol bioisosteres are described herein.
Stiff
Cory
C
Medicinal Chemistry, 301 Henrietta Street, Kalamazoo, MI 49001, USA.
Graber
David R
DR
Thorarensen
Atli
A
Wakefield
Brian D
BD
Marotti
Keith R
KR
Melchior
Earline P
EP
Sweeney
Michael T
MT
Han
Fusen
F
Rohrer
Douglas C
DC
Zurenko
Gary E
GE
Romero
Donna L
DL
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D018360:Crystallography, X-Ray; D007191:Indazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D015394:Molecular Structure; D014176:Protein Biosynthesis / Q000187:drug effects*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D062367:ortho-Aminobenzoates / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D007191:Indazoles; D062367:ortho-Aminobenzoates